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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Bicalutamide is typically used together with a GnRH analog or orchidectomy to treat advanced prostate cancer. In the UK, it is recommended by NICE for locally advanced prostate cancer at high risk of progression either alone or as adjuvant treatment to prostatectomy or radiotherapy. It is also recommended for locally advanced, nonmetastatic prostate cancer when surgical castration or other medical intervention are inappropriate, and for advanced prostate cancer in combination with a gonadorelin analog or surgical castration. It is also used in the treatment of hirsutism in women, as a component of feminizing hormone therapy for transgender women, and to treat early puberty in boys.
Development of palliative medicine in the United Kingdom and Ireland
Published in Eduardo Bruera, Irene Higginson, Charles F von Gunten, Tatsuya Morita, Textbook of Palliative Medicine and Supportive Care, 2015
35 Iversen P, Johansson JE, Lodding P et al. Bicalutamide 150mg in addition to standard care for patients with early non-metastatic prostate cancer: Updated from the Scandinavian Prostate Cancer Period Group-6 Study after a median follow-up period of 7.1 years. Scand J Urol Nephrol 2006; 40(6):441-452.
Utilizing clinical, pathological and radiological information to guide postoperative radiotherapy in prostate cancer
Published in Expert Review of Anticancer Therapy, 2023
Jerusha Padayachee, Simone Chaudhary, Brian Shim, Jonathan so, Remy Lim, Srinivas Raman
As discussed previously, despite early sPBRT, up to 30% of patients can still experience further biochemical relapse. There are ongoing investigations to further improve the outcomes of sPBRT, and an area that has drawn much interest is the use ADT. There have been three notable randomized trials that have suggested a benefit with the addition of ADT in this setting (Table 4). The RTOG 9601 trial reported by Shipley et al, evaluated the use of 2 years Bicalutamide versus placebo in 760 patients planned for sPBRT [64]. At a median follow-up of 13 years, the primary endpoint of overall survival (OS) favored the use of Bicalutamide (76.3% vs 71.3%, p = 0.04). In addition, incidence of prostate cancer-specific death, distant metastases, and a second biochemical relapse were reduced in the Bicalutamide arm (5.8% vs 13.4%, 14.5% vs 23%, 44% vs 67.9%; respectively). The most significant adverse effect with Bicalutamide use was gynecomastia, which was experienced in up to 70% of patients.
The Swedish national guidelines on prostate cancer, part 1: early detection, diagnostics, staging, patient support and primary management of non-metastatic disease
Published in Scandinavian Journal of Urology, 2022
Ola Bratt, Stefan Carlsson, Per Fransson, Camilla Thellenberg Karlsson, Johan Stranne, Jon Kindblom
In men with localised prostate cancer (cT1-2) with a moderately high PSA value (<30–50 ng/ml) and a PSA doubling time over 12 months, primary hormonal treatment does not prolong survival [48,49]. Watchful waiting is therefore the preferred management option for these patients if they are not candidates for curative treatment. In men with higher or more rapidly increasing PSA values and in men with locally advanced, non-metastatic disease, early hormonal treatment does prolong life, provided that their life expectancy is more than 5 years [48,49]. The Swedish guidelines recommend bicalutamide 150 mg once daily over GnRH agonists, based on bicalutamide’s more favourable side-effect profile [50,51], which the European guidelines do not. Single-dose breast irradiation should be given before the start of bicalutamide treatment [54].
Multivariate analysis in the development of bioequivalent tablets containing bicalutamide
Published in Pharmaceutical Development and Technology, 2021
Roman Goněc, Aleš Franc, Petr Doležel, Pavel Farkaš, Petr Sova
Bicalutamide is well absorbed following oral administration, although the absolute bioavailability is unknown. Since the molecule is non-ionic, neither the solubility nor the absorption is pH-dependent. Co-administered food has also no impact on the bioavailability. Long Tmax, exceeding 30 h, shows that not the dissolution rate but the total portion of dissolved bicalutamide is the limiting factor of bioavailability (Cockshot et al. 1997). That is the reason why poor solubility and dissolution are key factors limiting its oral bioavailability even though the absorption of bicalutamide is very good. Because the absorption of bicalutamide is not linear, there has to exist unknown absorption mechanism for bicalutamide in human organism (Cockshot 2004). To increase the solubility of poorly soluble drugs in oral solid drug forms, either special manufacturing procedures (Okáčová et al. 2011) or special formulations (Okáčová et al. 2010) can be used.